Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors
Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors
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DOI：
10.1016/s0960-894x(03)00588-2
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发表时间：
2003-09-01
影响因子：
2.7
通讯作者：
Chamberlin, AR
中科院分区：
文献类型：
--
作者：
Gulledge, BM;Aggen, JB;Chamberlin, AR
合成并筛选了一系列大大简化的微囊藻毒素类似物，仅包含 Adda（微囊藻毒素、节球菌素和莫图孔蛋白共有的 β-氨基酸）和单个附加氨基酸残基，并筛选用于抑制蛋白磷酸酶 I 和 2A。一些类似物被证明是酶的中纳摩尔抑制剂。 (C) 2003 年，爱思唯尔有限公司出版。
A series of greatly simplified microcystin analogues comprised only of Adda (the beta-amino acid common to the microcystins. nodularins, and motuporin,) and a single additional amino acid residue was synthesized and screened for inhibition of the protein phosphatases I and 2A. Several of the analogues were shown to be mid-nanomolar inhibitors of the enzymes. (C) 2003 Published by Elsevier Ltd.